Active substanceEthyl methylhydroxypyridine succinate + [Pyridoxine]Ethyl methylhydroxypyridine succinate + [Pyridoxine]
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  • Mexico 6®
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substances: ethylmethyl hydroxypyridine succinate 125 mg, pyridoxine hydrochloride 10 mg;

    Excipients: calcium hydrogen phosphate dihydrate 65 mg, calcium stearate 6.7 mg, copovidone 14 mg, silicon dioxide colloid 20 mg, croscarmellose sodium 20 mg, magnesium lactate dihydrate 327.6 mg, magnesium stearate 6.7 mg, hydrogenated castor oil 5 mg, cellulose microcrystalline 50 mg;

    composition of film shell: Fill white with 20 mg, including: hypromellose (hydroxypropylmethylcellulose) 6.75 mg, giprolose (hydroxypropyl cellulose) 6.75 mg, talc 4 mg, titanium dioxide 2.5 mg.

    Description:

    Round, biconvex tablets, covered with a film shell of white or almost white color. On a cross-section - white or almost white color.

    Pharmacotherapeutic group:Antioxidant + Vitamin
    ATX: & nbsp

    N.07.X.X   Other drugs for the treatment of diseases of the nervous system

    Pharmacodynamics:

    Ethyl methylhydroxypyridine succinate inhibitor free radical processes - membranoprotector, which also possesses antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic action.

    Antioxidant drug, regulating metabolic processes in the myocardium and vascular wall. The mechanism of action is due to antioxidant and membrane-protective properties. Suppresses peroxide oxidation of lipids, increases the activity of superoxidease, affects the physicochemical properties (phosphotidylserine and phosphotidylinosit, etc.) in the membrane, reduces the ratio of cholesterol / phospholipids, reduces the viscosity of the lipid layer and increases fluidity of the membrane, activates the energy-producing functions of mitochondria, and improves energy metabolism in the cell and thus protects the apparatus cells and the structure of their membranes. The change in the functional activity of the biological membrane caused by the drug leads to conformational changes in the protein macromolecules of synaptic membranes, as a result of which it has a modulating effect on the activity of membrane-bound enzymes, ion channels and receptor complexes,in particular, benzodiazepine, GABA, acetylcholine, enhancing their ability to bind to ligands, increasing the activity of neurotransmitters and activation of synaptic processes.

    Enhances the compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under conditions of hypoxia with an increase in adenosine triphosphate (ATP) and creatine phosphate, activates the energy-producing function of mitochondria.

    Increases the resistance of the body to the effects of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebral circulation disorders, intoxication with ethanol and antipsychotic drugs). It improves the metabolism and blood supply of the brain, microcirculation and rheological properties of blood, reduces platelet aggregation.

    Stabilizes the membranes of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis. Has hypolipidemic action, reduces the content of total cholesterol and low density lipoprotein (LDL).

    Improves the functional state of the ischemic myocardium,reducing the manifestations of systolic and diastolic dysfunction of the left ventricle (LV), as well as electrical instability of the myocardium.

    In conditions of a critical decline in coronary blood flow, structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes of phosphodiesterase, adenylate cyclase, acetylcholinesterase. It supports the activation of aerobic glycolysis in acute ischemia and promotes the reduction of mitochondrial oxidation-reduction processes in hypoxic conditions, increases the synthesis of adenosine triphosphate (ATP), creatine phosphate and other macroerges. Increases the collateral blood supply of the ischemic myocardium and activates the energosynthesizing processes in the ischemic zone, which contributes to maintaining the integrity of the cardiomyocytes and maintaining their functional activity.

    Patients with stable angina increases exercise tolerance nitrates and anti-anginal activity, improves the rheological properties of the blood, reduces the incidence of acute coronary insufficiency.

    Pyridoxine, entering the body, phosphorylated, converted to pyridoxal-5-phosphate and is part of the enzymes that carry out decarboxylation, transamination and racemization of amino acids, as well as enzymatic conversion sulfur-containing and hydroxylated amino acids. Participates in the metabolism; is necessary for the normal functioning of the central and peripheral nervous system. Pyridoxine participates in the exchange of tryptophan, methionine, cysteine, glutamic and other amino acids. It plays an important role in the exchange of histamine. Promotes the normalization of lipid metabolism.

    Pharmacokinetics:

    Ethyl methylhydroxypyridine succinate quickly absorbed when taken orally (period

    semiabsorption - 0.08-1 h). The time to reach the maximum concentration (TfrommOh) for oral administration - 0.46-0.5 hours. The maximum concentration (CmOh) when administered orally - 50-100 ng / ml. Quickly distributed in organs and tissues. Average hold time

    ethylmethylhydroxypyridine succinate in the body when ingested - 4.9-5.2 hours.

    Ethyl methylhydroxypyridine succinate is metabolized in the liver by glucuronation.

    5 metabolites were identified: 3-hydroxypyridine phosphate - formed in the liver andparticipation of alkaline phosphatase decomposes into phosphoric acid and 3-hydroxypyridine; The second metabolite is pharmacologically active, is formed in large quantities and is found in the urine on the 1-2 day after administration; 3rd - is excreted in large quantities with urine; 4-th and 5-th - glucuronconjugates. The half-life with oral administration is 4.7-5 hours. It is rapidly excreted in the urine mainly in the form of metabolites (50% for 12 hours) and in an insignificant amount in unchanged form (0.3% per 12 hours). The most intense withdrawal during the first 4 hours after taking ethylmethylhydroxypyridine succinate. The urinary excretion of unchanged ethylmethyl hydroxypyridine succinate and metabolites has a significant individual variability.

    Pyridoxine absorbed rapidly throughout the small intestine. Metabolized in the liver with the formation of pharmacologically active metabolites (pyridoxalphosphate and pyridoxamino phosphate). Pyridoxalphosphate with plasma proteins binds to 90%.

    It penetrates well into all tissues; accumulates mainly in the liver, less - in the muscles and central nervous system (CNS). Penetrates through the placenta, is secreted with breast milk. Half-life (T1/2) - 15-20 days. It is excreted by the kidneys (with intravenous injection - with bile 2%), as well as during hemodialysis.

    Indications:

    In the combination therapy:

    - discirculatory encephalopathy;

    - a syndrome of vegetative dystonia;

    - anxiety states in neurotic and neurosis-like states;

    - abstinence syndrome with alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;

    - ischemic heart disease (prevention of seizures);

    - state after acute intoxication by antipsychotic drugs;

    - asthenic conditions, and also for the prevention of the development of somatic diseases under the influence of extreme factors and loads;

    - influence of extreme (stressor) factors.

    Contraindications:

    - Hypersensitivity;

    - Acute hepatic and / or renal insufficiency;

    - Pregnancy, lactation;

    - childhood.

    Carefully:

    Stomach ulcer and duodenal ulcer.

    Dosing and Administration:

    Inside, 1 tablet 3 times a day; the initial dose of 1-2 tablets 1-2 times a day with a gradual increase to obtain a therapeutic effect. The maximum daily dose of 6 tab / day. Duration of treatment is 2-8 weeks.If necessary, it is possible to conduct repeated courses.

    Side effects:

    Nausea, dry mouth, diarrhea, drowsiness, allergic reactions, hypersecretion of hydrochloric acid (HCl), numbness, the appearance of a feeling of compression in the limbs - a symptom of "stocking" and "gloves," a decrease in lactation (sometimes it is used as a therapeutic effect).

    Overdose:

    Ethyl methylhydroxypyridine succinate

    Due to low toxicity, an overdose is unlikely. In case of an accidental overdose, drowsiness and sedation may occur. Treatment, as a rule, is not required - the symptoms disappear on their own within a day. In severe cases with insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.

    Pyridoxine

    Taking high doses of pyridoxine for a short period of time (at a dose of more than 1 g per day) can lead to a short-term occurrence of neurotoxic effects.

    When taking pyridoxine in a dose exceeding 150 mg / kg body weight, it is recommended to induce vomiting and take Activated carbon. Provocation of vomiting is most effective during the first 30 minutes after taking the drug. Emergency measures may be required.

    Interaction:

    Ethyl methylhydroxypyridine succinate

    Enhances the action of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian drugs (levodopa), nitrates. Reduces the toxic effects of ethanol.

    Pyridoxine

    Strengthens the action of diuretics, weakens the activity of levodopa, it goes well with cardiac glycosides (pyridoxine promotes an increase in the synthesis of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate (increases resistance to hypoxia).

    Pyridoxine is pharmaceutically incompatible with thiamine and cyanocobalamin. Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Tablets, film-coated, 125 mg + 10 mg.
    Packaging:

    For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    According to 1, 2, 3, 6, 10 contour cell packs of 10 tablets or 1, 2, 4, 6 contour cell packs of 15 tablets together with the instruction for use are placed in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008177/10
    Date of registration:17.08.2010 / 10.07.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp26.04.2018
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